Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1995-01-24
1998-06-16
MacMillan, Keith
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
A61K 31195
Patent
active
057671591
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION OF THE INVENTION
The invention relates generally to a preparation for increasing muscle performance ability in mammals having no disorders in creatine metabolism, and thereby increasing muscular strength, shortening the period of re-establishment of phosphorous compounds in energy after work and increasing the body of the muscles. This is achieved by the administration of creatine to the mammals in an amount of at least 15 grammes, or 0.2-0.4 g/kg body weight or preferably about 0.3 g/kg body weight, per day for at least 2 days. The invention describes the use of creatine for the manufacturing of a prepara- tion comprising creatine in an amount which supplies a daily dose as stated above, as well as a method for increasing muscle per- formance ability in mammals having no disorder in creatine metabolism by supplying a daily dosage of at least 15 grammes, or 0.3 g/kg body weight, optionally divided in several doses.
BACKGROUND OF THE INVENTION
It is well established that creatine phosphate is the substrate in muscular tissue which gives the fastest resynthesis of ATP (adenosine triphosphate) and through this is used at maximum or nearly maximum power production. The resynthesis speed of ATP is nearly twice as high from creatine phosphate than from glycogen (the carbohydrate in muscle) and we have been able to show that muscle contraction with maximum power depletes the creatine phosphate supply (Hultman et al Biochem. Soc. Trans 1991; 19, 347-354). Even the oxidative resynthesis of energy substrate after work is effected positively by increased creatine amounts in the muscle tissue. It has therefore been suggested that a positive relationship exists between the amount of creatine in the muscle and the power production on repeated work with short breaks for resting.
Creatine is not sythesized in muscle tissue but is supplied to the muscle via the blood stream - partly from synthesis in liver, kidney and pancreas, and partly from the intake via food. The blood concentration of creatine is in the order of 50 .mu.mol per liter blood and from this level a creatine uptake to the muscle tissue takes place via an active transport. The creatine excretion in the form of creatinine varies with the size of the muscle mass and reaches 0.2-2 g per day in a normal weight person.
Attempts have been made to improve the muscle power by increasing the creatine content in muscle. Creatine has been administered in different forms and in combination with other substances in different forms and in combination with other substances, such as Royal Jelly, carnosine, vitamins and amino acid compounds. Also creatine phosphate has been administered. In these attempts daily doses corresponding to 100 mg up to several grammes have been administered. This method of dosage of creatine produces moderate increases in the blood level of creatine but no measurable increases of the creatine content of the muscle (own experiments).
EP 199 117 discloses phosphocreatine as active ingredient in a parenteral preparation for the treatment of cardiac infarct and to protect the cardiac muscle (myocardium) during heart surgery. The preparation is stated to comprise 3-35 mmol disodium phosphocreatine. Example 3 discloses the use of 6 g phosphocreatine day 1 and thereafter treatment with 2 g/day during day 1 to 7.
EP 222 257 discloses compositions containing phosphocreatine to be used in therapy against cardiac diseases in amounts of 200 to 400 mg/kg/day.
WO 91/07954 relates to the use of guanidino acetic acid as a creatine precursor to achieve high intracellular muscular content of creatine in the skeletal and cardiac muscular cells. However, the applicant states at p. 2, lines 14 to 18, that "the administration of exogenous creatine does not bring any positive result, because exogenous creatine inhibits the synthesis of endogenous creatine for a quantity equal to the quantity of the creatine administered.
From U.S. Pat. No. 5,091,404 a method is previously known for preserving and/or restoring the physiological function of in vivo animal
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Harris Roger C.
Hultman Eric
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